This invention relates to inducing anorexia in warm-blooded animals by administering nalbuphine or nalmetrene orally thereto.
Nalbuphine, otherwise known as 17-cyclobutyl-methyl-4,5.alpha.-epoxymorphinan-3,6.alpha.,14-triol, is known to possess both analgesic and narcotic antagonist activity. The compound and methods for preparing it are described in Pachter et al., U.S. Pat. No. 3,393,197, the disclosure of which is hereby incorporated by reference. The pharmacology of nalbuphine is reviewed by Miller, Am. J. Hosp. Pharm., 37, 942-9 (1980).
Nalmetrene is the common name for the compound 17-cyclopropylmethyl-4,5.alpha.-epoxy-6-methylenemorphinan-3,14-diol. This compound is known to be a potent narcotic antagonist and is disclosed in Fishman, U.S. Pat. Nos. 3,814,768 and 3,896,226, the disclosures of which are hereby incorporated by reference.
Smith, U.S. Pat. No. 4,217,353, which issued on Aug. 12, 1980, discloses that another narcotic antagonist, naltrexone ((-)-17-cyclopropylmethyl-4,5.alpha.-epoxy-3,14-dihydroxymorphinan-6-one), can be administered orally to effect appetite suppression in mammals. Holtzman, J. Pharmacol. Exp. Ther., 189, 51-60 (1974), has shown that the narcotic antagonist naloxone (N-allyl-14-hydroxy-7,8-dihydronormorphinone) suppresses eating by food-deprived rats but not by food-deprived mice. In a subsequent study, Holtzman showed that the fluid intake (sweetened Enfamil) of rats was reduced following subcutaneous administration of naloxone, naltrexone or nalorphine (N-allylnormorphine); Life Sciences, 16, 1465-70 (1975).
There is no indication in the known art that either nalbuphine or nalmetrene would be an effective appetite suppressant. In addition, the art does not disclose anorexigenic activity for any mixed agonist/antagonists such as nalbuphine.